no-losartan a

Angiotensin II is a hormone that plays an important role in regulating blood pressure. Elevated levels of angiotensin II are implicated in inducing and maintaining hypertension, and also in the development of atherosclerosis. Both of these effects are mediated by the angiotensin II type 1 (AT1) receptor. Losartan is a mammalian AT1 receptor antagonist with a Ki value of 5-20 nM. In humans, losartan effectively controls hypertension while protecting renal function. Nitric oxide (NO) causes vasodilation and also inhibits platelet and neutrophil aggregation in the endothelium. NO-losartan A possesses similar anti-hypertensive effects to losartan, with the addition of the vasodilating effects of NO release.

UR-7247 是一种新型可口服活性的血管紧张素 II 亚型 I（AT1）受体拮抗剂，具有显著持久的药效。体内研究显示，给药后 4 小时，10 mg UR-7247 与 100 mg losartan 在药效上无显著差异，而体外研究则显示 100 mg losartan 的阻断能力超过 UR-7247，提示 UR-7247 具有较长血浆半衰期，可能与其高亲和力蛋白结合有关，表明其在健康受试者中呈现出长效且耐受性良好的 AT1 阻断作用。